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Of Specific
Local Anesthetics
Based on Text- Local Anesthesia for Dental Professionals
1st ed. Dr. StanleyMalamed 2nd ed. Bassett, DiMarco, Naughton
Local Anesthesia for Dental Professionals
ο‚— Individual response to LA
ο‚— Bell shaped curve – normal responder
ο‚— Accuracy of deposit of LA - injection target
ο‚— Tissue pH
ο‚— Anatomic Variation
ο‚— Type of injection (block or infiltration)
ο‚— Normoresponders
ο‚— Average patient no
problem
ο‚— Hyperresponder
ο‚— LA more effective longer
and possibly quicker
ο‚— Hyporesponders
ο‚— LA less effective, shorter
and slow onset
ο‚— IANB
ο‚— Technique sensitive
ο‚— Anatomic variation
ο‚— Infiltration
ο‚— Easier to place solution
ο‚— Dissipation of solution
helps
ο‚— Influences onset and duration
ο‚— Inflammation, infection, and
pain decreases depth and
duration
ο‚— Increased vascularity of site
ο‚— Low pH more cations
ο‚— and slower dissociation into
axon
ο‚— Height of mandibular
foramen
ο‚— Width of ramus
ο‚— Bifid inferior alveolar nerve
ο‚— Accessory nerves
ο‚— Sensory innervation by
lingual and mylohyoid
nerves
ο‚— Type of injection influences the duration
ο‚— Nerve Block
ο‚— Longer duration
ο‚— Infiltration
ο‚— Shorter duration
ο‚— Less than recommended volumes will decrease onset
and duration
ο‚— Larger doses do not increase duration
ο‚— Related as mg/kg or mg/lb
ο‚— Normoresponders
ο‚— Maximum dose based on body weight
ο‚— Produces a LA blood level below usual threshold for an
overdose or toxic reaction
ο‚— Response is usually mild – tremor or drowsiness
ο‚— Hyporesoponders
ο‚— May not experience adverse Rxn until LA level is
considerably above the normal overdose
ο‚— Hyperresponder
ο‚— May demonstrate clinical signs of LA
ο‚— overdose At blood levels significantly lower than normal
ο‚— Always minimize the amount of LA
ο‚— Smallest clinical effective dose
88 mg / 36 mg carpule = 2.4
ο‚— Risk groups
ο‚— DECREASE DRUG DOSAGE
ο‚— Geriatric
ο‚— Medically compromised and organ functions diminished
ο‚— Pediatric
ο‚— Not fully developed and light weight is easy to overdose
ο‚— May be a hyperresponder
ο‚— Hepatic disease
ο‚— Do not metabolize drug normally
ο‚— Half life of drug increased
ο‚— If met or exceeded
ο‚— does NOT guarantee an overdose
ο‚— Hyper responders
ο‚— may OD at doses lower than MRD
ο‚— Lidocaine 2%
ο‚— MRD is 3.2 mg/lb
ο‚— or 500 mg. maximum
ο‚— 100 lb. patient
ο‚— MRD = 100 lb x 3.2 mg/lb= 320 mg
ο‚— Cartridge 1.8 ml x 20 mg/ml = 36 mg/cartridge
ο‚— #cartridges under MRD
ο‚— 320 mg MRD divided by 36 mg/ cartridge
ο‚— 8.8 cartridges for 100 lb patient
ο‚— Articaine 4%
ο‚— MRD is 3.2 mg / lb
ο‚— Dose = 1.7 ml x 40 mg/ml = 68 mg / cartridge
ο‚— 90 lb patient
ο‚— 90 lb x 3.2 mg/lb = 288 mg MRD
ο‚— # cartridges under MRD
ο‚— 288 mg MRD divided by 68 mg/cartridge
ο‚— 4.2 cartridges for 90 lb patient
ο‚— Mepivicaine 3%
ο‚— MRD is 3.0 mg/lb
ο‚— Dose / vial = 1.8ml x 30 mg/ml = 54 mg/cargridge
ο‚— 20 kg patient (20 kg x 2.2 lbs/kg = 44 lbs)
ο‚— 44 lbs x 30 mg/lb = 132 mg MRD
ο‚— # cartridges under MRD
ο‚— 132 mg divided by 54 mg/cartridge
ο‚— 2.4 cartridges for 44 lb patient
1 kg = 2.2 lbs
ο‚— Calculate MRD for each LA
ο‚— The lowest MRD is the safe threshold
ο‚— Both LA added together
ο‚— must be under the lowest MRD
ο‚— Mepivicaine 2% w/levonordefrin 1:20,000
ο‚— MRD is 3mg/lb
ο‚— Mepivicaine 2% = 36 mg / carpule
ο‚— 45 kg patient - 45 x 2.2 = 99 lbs
ο‚— MRD is 99 lbs x 3 mg / lb = 297 mg.
ο‚— 2 cartridges = 72 mg
ο‚— Articaine 4% = 68 mg / carpule
ο‚— MRD is 3.2 mg/lb
ο‚— 99 lb patient - 99 x 3.2 = 317 mg
ο‚— LOWEST MRD = MEPIVICAINE = 297 MG
ο‚— 297 mg - 72 mg mepivicaine = 225 mg of MRD remaining
ο‚— 225 mg divided by 68 mg/carpule = 3 carpules may be used
45 kg x 2.2 lb/kg = 99 lbs
ο‚— Hydrolyzed by blood plasma pseudocholinesterase
ο‚— Metabolites
ο‚— PABA – para-aminobenzoic acid – allergic rxns
ο‚— Diethylaminoethanol
ο‚— Excreted in kidneys
ο‚— Vasodilator action on blood vessels
ο‚— Lidocaine
ο‚— Articaine (hybrid)
ο‚— Mepivicaine
ο‚— Bupivicaine
Amide
ο‚— Lidocaine
ο‚— Articaine
ο‚— Mepivicaine
ο‚— Prilocaine
ο‚— Bupivicaine
ο‚— Dibucaine
ο‚— Etidocaine
ο‚— Cocaine
ο‚— Benzocaine
ο‚— Tetracaine
Esther (Topical use)
ο‚— Amide
ο‚— Metabolized in liver by
microsomal oxidases &
amidases
ο‚— Pregnancy category B
ο‚— Excretion by kidneys
ο‚— MRD
ο‚— 3.2 mg / lb
ο‚— 7 mg / kg
ο‚— Allergy to amide LA is nearly nonexistent
ο‚— Safe when used properly
ο‚— Available in 2% with
ο‚— 1:50,000 epi
ο‚— 1:100,000 epi
ο‚— Vasoconstrictor
ο‚— Decreases blood flow due to
ο‚— alpha adrenergic constriction (epinephrine = vasoconstrict)
ο‚— Distribution is slowed due to slower absorption into bv
ο‚— Increases depth and duration of LA
ο‚— Reduces blood level of LA
ο‚— Vasoconstrictor
ο‚— Decreases blood flow due to alpha adrenergic action to
cause constriction
ο‚— Distribution is slowed due to slower absorption into BV
ο‚— Increases depth and duration of LA
ο‚— Reduces blood level of LA
ο‚— MRD for vasoconstrictor – epinephrine driven
ο‚— ASA 3 – 4o micrograms / appt
ο‚— Epi 1:100,000 = .01 mg / ml x 1.8 ml = .018 mg /
carpule
ο‚— .04 mg divided by .018 mg/ carpule = 2 cartridges
ο‚— Amide
ο‚— Metabolized in liver
ο‚— by microsomal oxidases
ο‚— Excretion by kidneys
ο‚— Slight vasodilation
ο‚— Pregnancy category C
ο‚— Duration : 20-40 minutes
ο‚— Concentrations
ο‚— 3% without constrictor
ο‚— 2% with vasoconstrictor
ο‚— Mepivicaine plain
ο‚— Frequently used in pediatrics and geriatrics
ο‚— 3% without vasoconstrictor
ο‚— Recommended for patients
ο‚— with vasoconstrictor contraindications
ο‚— Provides depth and duration
ο‚— Due to vasoconstrictor levonordefrin
ο‚— Allergy is rare to non-existant
ο‚— Overdose signs
ο‚— Stimulation followed by depression
ο‚— Drowsiness to loss of consciousness
ο‚— Possible to have absence of stimulation
ο‚— Amide
ο‚— Secondary amine
ο‚— Metabolism by hepatic amidases into
ο‚— Orthotoluidine
ο‚— can induce methemoglobinemia
ο‚— N - propylalanine
ο‚— Excretion – kidneys
ο‚— Pregnancy category B
ο‚— Greater vasodilation than mepivicaine
ο‚— and less vasodilation than xylocaine
ο‚— Consistently reduces blood
oxygen carrying capacity
ο‚— Can cause cyanosis
ο‚— Limit total dose to 600 mg
ο‚— Plasma levels of prilocaine
decrease faster than
lidocaine
ο‚— Thus is considered less
toxic
ο‚— Maximum Dose - 4 mg/lb
ο‚— To maximum of 600 mg.
ο‚— Can provide anesthesia equal duration to
ο‚— Lidocaine or mepivocaine with epinephrine
ο‚— Relatively contraindicated in patients with
ο‚— Methemoglobinemia
ο‚— Hemoglobinopathies (sickle cell anemia)
ο‚— Congestive heart failure (CHF)
ο‚— Respiratory failure
ο‚— Acetaminophen or phenacetin that elevate
methemoglobin
ο‚— Eutectic mixture of LA
ο‚— Lidocaine
ο‚— Prilocaine
ο‚— Penetrates skin –
ectodermis
ο‚— In uncharged base form
ο‚— Hybrid molecule – both esther and amide
ο‚— Metabolism
ο‚— plasma esterase
ο‚— and hepatic microsomal enzymes
ο‚— Excretion – kidneys
ο‚— Vasodilation equal to lidocaine
ο‚— Pregnancy class C
ο‚— Maximum dose
ο‚— 7 mg/kg (3.2 mg/lb)
ο‚— Only amide
ο‚— to possess thiophene ring making it lipid soluble
ο‚— Has a Sulphur atom
ο‚— Contraindication - If patient allergic to sulfur
ο‚— IV doses can cause methemoglobinemia
ο‚— Not recommended in age 4 or younger & geriatrics
ο‚— Contraindicated with amide allergy
ο‚— Preservative sodium metabisulfite
ο‚— Contraindication - persons with sulfite sensitivity
ο‚— Patients with allergic type asthma
ο‚— Amide
ο‚— Related to mepivicaine
ο‚— Butyl group replaces methyl
ο‚— 400% more potent than lidocaine (4x)
ο‚— 400% less toxic than lidocaine and mepivicaine
ο‚— Metabolized in liver by amidases
ο‚— Excretion by kidneys 16% unchanged
ο‚— Vasodilating
ο‚— greater than lidocaine, prilocaine and mepivicaine
ο‚— Pregnancy Class C
ο‚— Maximum recommended dose 90 mg
ο‚— No dose based on body weight
ο‚— .5% concentration
ο‚— 1:200,000 epi
ο‚— Indications
ο‚— Lengthy dental appointments needing 90 minutes LA
ο‚— Management of post op pain
ο‚— DIMINISHES NEED FOR OPOIDS
ο‚— Not recommended
ο‚— Hepatic disease
ο‚— Amide allergy
ο‚— Younger patients
ο‚— Those who could injure themselves by biting their lip
ο‚— Mentally disabled, young, geriatric
ο‚— Length of time - duration
ο‚— Post treatment pain control
ο‚— .5% bupivicaine 8-12 hours soft tissue anesthesia
ο‚— Risk for young and old whose cognitive ability is limited
ο‚— Bite their lip, cheek, or tongue
ο‚— 3% mepivicaine may be better
ο‚— Hemostasis
ο‚— Vasoconstrictor 1:50,000 or 1:100,000 epi
ο‚— 1:200,000 concentrations are not effective for hemostasis
ο‚— Absolute
ο‚— Not administered ever
ο‚— Life threatening risk unacceptable
ο‚— Medical contraindication
ο‚— True documented allergy
ο‚— Relative
ο‚— Preferable to avoid LA in question
ο‚— The risk of adverse reaction is increased
ο‚— Seek an alternative LA
ο‚— If acceptable alternative is not available may be used
with caution
ο‚— Amides are preferred to esters whenever possible
ο‚— Due to safety margin
ο‚— Fewer allergic reactions
ο‚— Decreased risk of methemoglobinemia
ο‚— β€œAtraumatic”
administration of
injections
ο‚— Topical typically will not
diffuse thru epidermis
ο‚— Will penetrate mucous
membrane or abraided
skin
ο‚— Higher concentration (more base molecule)
ο‚— May be 7.5% and up to 15% concentration
ο‚— Promotes diffusion thru mucous membrane
ο‚— Increases toxicity
ο‚— Vasodilating properties and absorption can be rapid
ο‚— Dose is important
ο‚— Blood levels can rise rapidly to IV levels of admin.
ο‚— Typically active 2-3 mm deep only
ο‚— Allows atraumatic needle penetration
ο‚— Insoluble in water
ο‚— Soluble in
ο‚— alcohol, propylene glycol and polyethylene glocol
ο‚— Vehicles for surface application
ο‚— Esther
ο‚— Poor solubility in water
ο‚— Overdose or systemic reaction is unknown
ο‚— Localized allergic reaction can occur
ο‚— Remains at site of application longer
ο‚— prolonged duration
ο‚— Inhibits antibacterial action of sulfonamides
ο‚— Ketone Derivative
ο‚— Without esther or amide linkage
ο‚— May be used in patients allergic to common LA
ο‚— Cross sensitization with other LA doesn’t occur
ο‚— Potency equal to cocaine
ο‚— Onset slow - 10 minutes
ο‚— Duration long – 1 hour
ο‚— Toxicity is extremely low due to water insolubility
ο‚— .5 % used in dentistry
ο‚— Lidocaine 5% base
ο‚— Spray, ointment, patch and solution
ο‚— Poorly water soluble- used on open wound / skin
ο‚— Lidocaine HCl
ο‚— water soluble – in topical solution 20 0r 40 mg/ml
ο‚— Penetrates tissue more effectively than base form
ο‚— Greater absorption and risk of toxicity
ο‚— Maximum recommended dose 200 mg
ο‚— Long duration esther LA
ο‚— Highly soluble in water
ο‚— Topically is 5-8 x more
potent than cocaine
ο‚— Onset slow and duration
about 45 minutes
ο‚— Metabolized in plasma by
estherases
ο‚— Maximum dose topically is
20 mg
ο‚— Greater potential for
systemic toxicity
ο‚— A sterile gauze wipe
should be used to
prepare tissues prior to
injection
ο‚— Helps reduce post
injection infections
ο‚— Minimal quantity of topical on applicator tip
ο‚— Applied directly to site
ο‚— Allow 1 minute
ο‚— Studies state 10 – 15 seconds is adequate
ο‚— but patients feel rushed
ο‚— 2-3 minutes gives profound tissue topical anesthesia
ο‚— Benzocaine – ester - is not
absorbed systemically
ο‚— Local reactions only =
angioneurotic edema of lips
ο‚— Lidocaine - amide –
topical anesthesia
ο‚— Greater risk due to
systemic absorption
ο‚— EMLA effective for
intraoral but not designed
for this
Ester allergy
Angioneurotic edema
ο‚— Eutectic Mixture of Local Anesthetics
ο‚— Lidocaine 2.5% + Prilocaine 2.5%
ο‚— Surface anesthesia for intact skin
ο‚— Contraindication
ο‚— Methemoglobinemia
ο‚— Amide sensitivity
ο‚— Younger than 12 months with treatment by
methemoglobin inducing agents
ο‚— Not recommended for use on mucous membranes
ο‚— More rapid onset
ο‚— Greater depth of penetration
ο‚— Higher concentration of base molecules
ο‚— Because of prilocaine
ο‚— Risk of methemoglobinemia
ο‚— Both are amides, eutectic mixture @ 2.5%
ο‚— Onset in 1 minute
ο‚— Duration 14 – 13 minutes
ο‚— Designed for intrapocket use
ο‚— Liquid at room temperature
ο‚— thickens to gel subgingivally
ο‚— Syringe with blunt tip applicator
ο‚— Low systemic toxicity
ο‚— 20-40% of drug systemic
ο‚— Unmetered – NOT recommended
ο‚— Metered dose – may be used
ο‚— If a continuous spray is used
ο‚— Rapid absorption
ο‚— May reach OD levels quickly
ο‚— Spray nozzle must be changed
Local Anesthesia for Dental Professionals - Clinical  action of specific la
Local Anesthesia for Dental Professionals - Clinical  action of specific la
Local Anesthesia for Dental Professionals - Clinical  action of specific la
Local Anesthesia for Dental Professionals - Clinical  action of specific la

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Local Anesthesia for Dental Professionals - Clinical action of specific la

  • 1. Of Specific Local Anesthetics Based on Text- Local Anesthesia for Dental Professionals 1st ed. Dr. StanleyMalamed 2nd ed. Bassett, DiMarco, Naughton Local Anesthesia for Dental Professionals
  • 2. ο‚— Individual response to LA ο‚— Bell shaped curve – normal responder ο‚— Accuracy of deposit of LA - injection target ο‚— Tissue pH ο‚— Anatomic Variation ο‚— Type of injection (block or infiltration)
  • 3. ο‚— Normoresponders ο‚— Average patient no problem ο‚— Hyperresponder ο‚— LA more effective longer and possibly quicker ο‚— Hyporesponders ο‚— LA less effective, shorter and slow onset
  • 4. ο‚— IANB ο‚— Technique sensitive ο‚— Anatomic variation ο‚— Infiltration ο‚— Easier to place solution ο‚— Dissipation of solution helps
  • 5. ο‚— Influences onset and duration ο‚— Inflammation, infection, and pain decreases depth and duration ο‚— Increased vascularity of site ο‚— Low pH more cations ο‚— and slower dissociation into axon
  • 6. ο‚— Height of mandibular foramen ο‚— Width of ramus ο‚— Bifid inferior alveolar nerve ο‚— Accessory nerves ο‚— Sensory innervation by lingual and mylohyoid nerves
  • 7. ο‚— Type of injection influences the duration ο‚— Nerve Block ο‚— Longer duration ο‚— Infiltration ο‚— Shorter duration ο‚— Less than recommended volumes will decrease onset and duration ο‚— Larger doses do not increase duration
  • 8. ο‚— Related as mg/kg or mg/lb ο‚— Normoresponders ο‚— Maximum dose based on body weight ο‚— Produces a LA blood level below usual threshold for an overdose or toxic reaction ο‚— Response is usually mild – tremor or drowsiness ο‚— Hyporesoponders ο‚— May not experience adverse Rxn until LA level is considerably above the normal overdose
  • 9. ο‚— Hyperresponder ο‚— May demonstrate clinical signs of LA ο‚— overdose At blood levels significantly lower than normal ο‚— Always minimize the amount of LA ο‚— Smallest clinical effective dose
  • 10. 88 mg / 36 mg carpule = 2.4
  • 11. ο‚— Risk groups ο‚— DECREASE DRUG DOSAGE ο‚— Geriatric ο‚— Medically compromised and organ functions diminished ο‚— Pediatric ο‚— Not fully developed and light weight is easy to overdose ο‚— May be a hyperresponder ο‚— Hepatic disease ο‚— Do not metabolize drug normally ο‚— Half life of drug increased
  • 12.
  • 13. ο‚— If met or exceeded ο‚— does NOT guarantee an overdose ο‚— Hyper responders ο‚— may OD at doses lower than MRD
  • 14. ο‚— Lidocaine 2% ο‚— MRD is 3.2 mg/lb ο‚— or 500 mg. maximum ο‚— 100 lb. patient ο‚— MRD = 100 lb x 3.2 mg/lb= 320 mg ο‚— Cartridge 1.8 ml x 20 mg/ml = 36 mg/cartridge ο‚— #cartridges under MRD ο‚— 320 mg MRD divided by 36 mg/ cartridge ο‚— 8.8 cartridges for 100 lb patient
  • 15. ο‚— Articaine 4% ο‚— MRD is 3.2 mg / lb ο‚— Dose = 1.7 ml x 40 mg/ml = 68 mg / cartridge ο‚— 90 lb patient ο‚— 90 lb x 3.2 mg/lb = 288 mg MRD ο‚— # cartridges under MRD ο‚— 288 mg MRD divided by 68 mg/cartridge ο‚— 4.2 cartridges for 90 lb patient
  • 16. ο‚— Mepivicaine 3% ο‚— MRD is 3.0 mg/lb ο‚— Dose / vial = 1.8ml x 30 mg/ml = 54 mg/cargridge ο‚— 20 kg patient (20 kg x 2.2 lbs/kg = 44 lbs) ο‚— 44 lbs x 30 mg/lb = 132 mg MRD ο‚— # cartridges under MRD ο‚— 132 mg divided by 54 mg/cartridge ο‚— 2.4 cartridges for 44 lb patient 1 kg = 2.2 lbs
  • 17. ο‚— Calculate MRD for each LA ο‚— The lowest MRD is the safe threshold ο‚— Both LA added together ο‚— must be under the lowest MRD
  • 18. ο‚— Mepivicaine 2% w/levonordefrin 1:20,000 ο‚— MRD is 3mg/lb ο‚— Mepivicaine 2% = 36 mg / carpule ο‚— 45 kg patient - 45 x 2.2 = 99 lbs ο‚— MRD is 99 lbs x 3 mg / lb = 297 mg. ο‚— 2 cartridges = 72 mg ο‚— Articaine 4% = 68 mg / carpule ο‚— MRD is 3.2 mg/lb ο‚— 99 lb patient - 99 x 3.2 = 317 mg ο‚— LOWEST MRD = MEPIVICAINE = 297 MG ο‚— 297 mg - 72 mg mepivicaine = 225 mg of MRD remaining ο‚— 225 mg divided by 68 mg/carpule = 3 carpules may be used 45 kg x 2.2 lb/kg = 99 lbs
  • 19. ο‚— Hydrolyzed by blood plasma pseudocholinesterase ο‚— Metabolites ο‚— PABA – para-aminobenzoic acid – allergic rxns ο‚— Diethylaminoethanol ο‚— Excreted in kidneys ο‚— Vasodilator action on blood vessels
  • 20. ο‚— Lidocaine ο‚— Articaine (hybrid) ο‚— Mepivicaine ο‚— Bupivicaine
  • 21. Amide ο‚— Lidocaine ο‚— Articaine ο‚— Mepivicaine ο‚— Prilocaine ο‚— Bupivicaine ο‚— Dibucaine ο‚— Etidocaine ο‚— Cocaine ο‚— Benzocaine ο‚— Tetracaine Esther (Topical use)
  • 22. ο‚— Amide ο‚— Metabolized in liver by microsomal oxidases & amidases ο‚— Pregnancy category B ο‚— Excretion by kidneys ο‚— MRD ο‚— 3.2 mg / lb ο‚— 7 mg / kg
  • 23. ο‚— Allergy to amide LA is nearly nonexistent ο‚— Safe when used properly ο‚— Available in 2% with ο‚— 1:50,000 epi ο‚— 1:100,000 epi ο‚— Vasoconstrictor ο‚— Decreases blood flow due to ο‚— alpha adrenergic constriction (epinephrine = vasoconstrict) ο‚— Distribution is slowed due to slower absorption into bv ο‚— Increases depth and duration of LA ο‚— Reduces blood level of LA
  • 24. ο‚— Vasoconstrictor ο‚— Decreases blood flow due to alpha adrenergic action to cause constriction ο‚— Distribution is slowed due to slower absorption into BV ο‚— Increases depth and duration of LA ο‚— Reduces blood level of LA ο‚— MRD for vasoconstrictor – epinephrine driven ο‚— ASA 3 – 4o micrograms / appt ο‚— Epi 1:100,000 = .01 mg / ml x 1.8 ml = .018 mg / carpule ο‚— .04 mg divided by .018 mg/ carpule = 2 cartridges
  • 25. ο‚— Amide ο‚— Metabolized in liver ο‚— by microsomal oxidases ο‚— Excretion by kidneys ο‚— Slight vasodilation ο‚— Pregnancy category C ο‚— Duration : 20-40 minutes ο‚— Concentrations ο‚— 3% without constrictor ο‚— 2% with vasoconstrictor
  • 26.
  • 27. ο‚— Mepivicaine plain ο‚— Frequently used in pediatrics and geriatrics ο‚— 3% without vasoconstrictor ο‚— Recommended for patients ο‚— with vasoconstrictor contraindications
  • 28. ο‚— Provides depth and duration ο‚— Due to vasoconstrictor levonordefrin ο‚— Allergy is rare to non-existant ο‚— Overdose signs ο‚— Stimulation followed by depression ο‚— Drowsiness to loss of consciousness ο‚— Possible to have absence of stimulation
  • 29.
  • 30. ο‚— Amide ο‚— Secondary amine ο‚— Metabolism by hepatic amidases into ο‚— Orthotoluidine ο‚— can induce methemoglobinemia ο‚— N - propylalanine ο‚— Excretion – kidneys ο‚— Pregnancy category B ο‚— Greater vasodilation than mepivicaine ο‚— and less vasodilation than xylocaine
  • 31. ο‚— Consistently reduces blood oxygen carrying capacity ο‚— Can cause cyanosis ο‚— Limit total dose to 600 mg ο‚— Plasma levels of prilocaine decrease faster than lidocaine ο‚— Thus is considered less toxic ο‚— Maximum Dose - 4 mg/lb ο‚— To maximum of 600 mg.
  • 32. ο‚— Can provide anesthesia equal duration to ο‚— Lidocaine or mepivocaine with epinephrine ο‚— Relatively contraindicated in patients with ο‚— Methemoglobinemia ο‚— Hemoglobinopathies (sickle cell anemia) ο‚— Congestive heart failure (CHF) ο‚— Respiratory failure ο‚— Acetaminophen or phenacetin that elevate methemoglobin
  • 33. ο‚— Eutectic mixture of LA ο‚— Lidocaine ο‚— Prilocaine ο‚— Penetrates skin – ectodermis ο‚— In uncharged base form
  • 34. ο‚— Hybrid molecule – both esther and amide ο‚— Metabolism ο‚— plasma esterase ο‚— and hepatic microsomal enzymes ο‚— Excretion – kidneys ο‚— Vasodilation equal to lidocaine ο‚— Pregnancy class C ο‚— Maximum dose ο‚— 7 mg/kg (3.2 mg/lb)
  • 35.
  • 36.
  • 37. ο‚— Only amide ο‚— to possess thiophene ring making it lipid soluble ο‚— Has a Sulphur atom ο‚— Contraindication - If patient allergic to sulfur ο‚— IV doses can cause methemoglobinemia ο‚— Not recommended in age 4 or younger & geriatrics ο‚— Contraindicated with amide allergy ο‚— Preservative sodium metabisulfite ο‚— Contraindication - persons with sulfite sensitivity ο‚— Patients with allergic type asthma
  • 38. ο‚— Amide ο‚— Related to mepivicaine ο‚— Butyl group replaces methyl ο‚— 400% more potent than lidocaine (4x) ο‚— 400% less toxic than lidocaine and mepivicaine ο‚— Metabolized in liver by amidases ο‚— Excretion by kidneys 16% unchanged ο‚— Vasodilating ο‚— greater than lidocaine, prilocaine and mepivicaine
  • 39.
  • 40. ο‚— Pregnancy Class C ο‚— Maximum recommended dose 90 mg ο‚— No dose based on body weight ο‚— .5% concentration ο‚— 1:200,000 epi ο‚— Indications ο‚— Lengthy dental appointments needing 90 minutes LA ο‚— Management of post op pain ο‚— DIMINISHES NEED FOR OPOIDS
  • 41. ο‚— Not recommended ο‚— Hepatic disease ο‚— Amide allergy ο‚— Younger patients ο‚— Those who could injure themselves by biting their lip ο‚— Mentally disabled, young, geriatric
  • 42. ο‚— Length of time - duration ο‚— Post treatment pain control ο‚— .5% bupivicaine 8-12 hours soft tissue anesthesia ο‚— Risk for young and old whose cognitive ability is limited ο‚— Bite their lip, cheek, or tongue ο‚— 3% mepivicaine may be better ο‚— Hemostasis ο‚— Vasoconstrictor 1:50,000 or 1:100,000 epi ο‚— 1:200,000 concentrations are not effective for hemostasis
  • 43. ο‚— Absolute ο‚— Not administered ever ο‚— Life threatening risk unacceptable ο‚— Medical contraindication ο‚— True documented allergy ο‚— Relative ο‚— Preferable to avoid LA in question ο‚— The risk of adverse reaction is increased ο‚— Seek an alternative LA ο‚— If acceptable alternative is not available may be used with caution
  • 44. ο‚— Amides are preferred to esters whenever possible ο‚— Due to safety margin ο‚— Fewer allergic reactions ο‚— Decreased risk of methemoglobinemia
  • 45. ο‚— β€œAtraumatic” administration of injections ο‚— Topical typically will not diffuse thru epidermis ο‚— Will penetrate mucous membrane or abraided skin
  • 46. ο‚— Higher concentration (more base molecule) ο‚— May be 7.5% and up to 15% concentration ο‚— Promotes diffusion thru mucous membrane ο‚— Increases toxicity ο‚— Vasodilating properties and absorption can be rapid ο‚— Dose is important ο‚— Blood levels can rise rapidly to IV levels of admin. ο‚— Typically active 2-3 mm deep only ο‚— Allows atraumatic needle penetration
  • 47. ο‚— Insoluble in water ο‚— Soluble in ο‚— alcohol, propylene glycol and polyethylene glocol ο‚— Vehicles for surface application
  • 48. ο‚— Esther ο‚— Poor solubility in water ο‚— Overdose or systemic reaction is unknown ο‚— Localized allergic reaction can occur ο‚— Remains at site of application longer ο‚— prolonged duration ο‚— Inhibits antibacterial action of sulfonamides
  • 49. ο‚— Ketone Derivative ο‚— Without esther or amide linkage ο‚— May be used in patients allergic to common LA ο‚— Cross sensitization with other LA doesn’t occur ο‚— Potency equal to cocaine ο‚— Onset slow - 10 minutes ο‚— Duration long – 1 hour ο‚— Toxicity is extremely low due to water insolubility ο‚— .5 % used in dentistry
  • 50. ο‚— Lidocaine 5% base ο‚— Spray, ointment, patch and solution ο‚— Poorly water soluble- used on open wound / skin ο‚— Lidocaine HCl ο‚— water soluble – in topical solution 20 0r 40 mg/ml ο‚— Penetrates tissue more effectively than base form ο‚— Greater absorption and risk of toxicity ο‚— Maximum recommended dose 200 mg
  • 51.
  • 52. ο‚— Long duration esther LA ο‚— Highly soluble in water ο‚— Topically is 5-8 x more potent than cocaine ο‚— Onset slow and duration about 45 minutes ο‚— Metabolized in plasma by estherases ο‚— Maximum dose topically is 20 mg ο‚— Greater potential for systemic toxicity
  • 53. ο‚— A sterile gauze wipe should be used to prepare tissues prior to injection ο‚— Helps reduce post injection infections
  • 54. ο‚— Minimal quantity of topical on applicator tip ο‚— Applied directly to site ο‚— Allow 1 minute ο‚— Studies state 10 – 15 seconds is adequate ο‚— but patients feel rushed ο‚— 2-3 minutes gives profound tissue topical anesthesia
  • 55. ο‚— Benzocaine – ester - is not absorbed systemically ο‚— Local reactions only = angioneurotic edema of lips ο‚— Lidocaine - amide – topical anesthesia ο‚— Greater risk due to systemic absorption ο‚— EMLA effective for intraoral but not designed for this Ester allergy Angioneurotic edema
  • 56. ο‚— Eutectic Mixture of Local Anesthetics ο‚— Lidocaine 2.5% + Prilocaine 2.5% ο‚— Surface anesthesia for intact skin ο‚— Contraindication ο‚— Methemoglobinemia ο‚— Amide sensitivity ο‚— Younger than 12 months with treatment by methemoglobin inducing agents ο‚— Not recommended for use on mucous membranes
  • 57.
  • 58.
  • 59. ο‚— More rapid onset ο‚— Greater depth of penetration ο‚— Higher concentration of base molecules ο‚— Because of prilocaine ο‚— Risk of methemoglobinemia
  • 60. ο‚— Both are amides, eutectic mixture @ 2.5% ο‚— Onset in 1 minute ο‚— Duration 14 – 13 minutes ο‚— Designed for intrapocket use ο‚— Liquid at room temperature ο‚— thickens to gel subgingivally ο‚— Syringe with blunt tip applicator ο‚— Low systemic toxicity ο‚— 20-40% of drug systemic
  • 61. ο‚— Unmetered – NOT recommended ο‚— Metered dose – may be used ο‚— If a continuous spray is used ο‚— Rapid absorption ο‚— May reach OD levels quickly ο‚— Spray nozzle must be changed